Activatable fluorescence agents

These agents enable in vivo imaging of biological processes. Non-fluorescent (optically silent) in their native (quenched) state, they generate high levels of fluorescence through enzyme-mediated release of their fluorochrome.

Map the in vivo status of a disease

Follow progression and responses to potential therapeutics

Investigate specific enzyme activity profiles in real time

Elucidate protease panels and disease

Use with other imaging agents for complementary molecular reporting

Highly sensitive

A single enzyme cleaving multiple fluorescence agents results
in unprecedented signal to background ratios to achieve
several hundred-fold signal amplification

Application examples

Deep central pulmonary metastases: detection and measurement of disease and therapeutic response (ProSense)

Fluorescence quantification corresponds to tumor burden as assessed by visual examination, lung weight and histological analysis

Treated

Untreated

Image: Coronal slices taken at lung depth show a dramatic effect of treatment on tumor-related fluorescence.
Investigation: Four- to five- week old female BALB/c mice received a chemotherapeutic regimen of Doxycycline (15 mg/kg/d) beginning one day following 4T1 cell injection. On day 13, mice were injected with ProSense 750 and imaged 24 hours later.

Mouse arthritis models: Earlier disease detection, measurement and monitoring (ProSense)

ProSense detected arthritis before clinical indications were measurable

Image: Comparison of conventional paw thickness assessment and ProSense imaging
Investigation: Five- week old female BALB/c mice received arthrogen-CIA monoclonal antibody cocktail to induce arthritis. On day 3, mice were injected with LPS and ProSense 750 and imaged 24 hours later.

ProSense provided a 10-fold signal compared to healthy animals at the disease peak.

Image: Comparison of conventional paw thickness assessment (measured using calipers) and ProSense imaging
Investigation: Five- week old female BALB/c mice received arthrogen-CIA monoclonal antibody cocktail and LPS to induce arthritis. On day 7, mice were injected with ProSense 750 and imaged 24 hours later.

Detection of MMP activity in the inflammatory disease process (MMPSense 680)

Image: Coronal tomographic slice at the depth of the arthritic paws.
Investigation: An adult DBA/1J mouse was immunized with bovine collagen (CIA model) to induce joint-directed immune-mediated damage. After two weeks, MMP activity was detected by injection of MMPSense 680 and imaged after 24 hours

Detailed application notes for download:

ProSense

Quantitative In vivo Fluorescence Imaging of Cancer Metastasis to the Lung and Response to Therapy (2007) (529.9 kB)

Non-Invasive optical imaging of lung metastasis and response to cancer therapy (2006) (147.5 kB)

In vivo tomographic and endoscopic imaging of experimental orthotopic colorectal cancer (2006) (197.8 kB)

Correlation of ProSense imaging with protease expression and activity in a mouse model of arthritis (2004) (161.2 kB)

In vivo optical imaging of disease progression with ProSense, a protease-sensing activatible agent (2004) (173.0 kB)

MMPSense

Optical Imaging of MMPSense as a Biomarker of Matrix Metalloprotease Activity In Vivo (2007) (4.4 MB)

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